Assay Detail
Binding
CHEMBL665260
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of dihydrofolate reductase (DHFR) from Pneumocystis carinii(pc)
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Pneumocystis carinii |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase inhibitors and antitumor agents: synthesis and biological activities of 2,4-diamino-5-methyl-6-[(monosubstituted anilino)methyl] pyrido[2,3-d]pyrimidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.22 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL50514 | — | — | 1 | 7.89 |
| CHEMBL80066 | — | — | 1 | 7.64 |
| CHEMBL310880 | — | — | 1 | 7.54 |
| CHEMBL79922 | — | — | 1 | 7.52 |
| CHEMBL264386 | — | — | 1 | 7.46 |
| CHEMBL79347 | — | — | 1 | 7.43 |
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 7.42 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 7.38 |
| CHEMBL283518 | — | — | 1 | 7.36 |
| CHEMBL81119 | — | — | 1 | 7.33 |
| CHEMBL23416 | — | — | 1 | 7.26 |
| CHEMBL420224 | — | — | 1 | 7.20 |
| CHEMBL80070 | — | — | 1 | 7.16 |
| CHEMBL79123 | — | — | 1 | 7.10 |
| CHEMBL80065 | — | — | 1 | 7.09 |
| CHEMBL309966 | — | — | 1 | 7.08 |
| CHEMBL23532 | — | — | 1 | 7.07 |
| CHEMBL312348 | — | — | 1 | 7.02 |
| CHEMBL82975 | — | — | 1 | 7.00 |
| CHEMBL82924 | — | — | 1 | 6.98 |
| CHEMBL84457 | — | — | 1 | 6.93 |
| CHEMBL281803 | — | — | 1 | 6.67 |
| CHEMBL81820 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL50514 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL80066 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL310880 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL79922 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL264386 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL79347 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL7492 | PIRITREXIM | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL283518 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL81119 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL23416 | — | IC50 | = | 55.4 | nM | 7.26 |
| CHEMBL420224 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL80070 | — | IC50 | = | 68.9 | nM | 7.16 |
| CHEMBL79123 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL80065 | — | IC50 | = | 80.8 | nM | 7.09 |
| CHEMBL309966 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL23532 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL312348 | — | IC50 | = | 95.4 | nM | 7.02 |
| CHEMBL82975 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL82924 | — | IC50 | = | 104.5 | nM | 6.98 |
| CHEMBL84457 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL281803 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL81820 | — | IC50 | = | 320.0 | nM | 6.50 |